Dopamine Receptor: Novel Opportunities for Drug Developments
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 31 January 2026 | Viewed by 35
Special Issue Editors
Interests: medicinal chemistry; pharmaceutical chemistry; GPCR; molecular modelling; ADMET studies
Interests: receptor chemistry; drug discovery; biologically active ligands; structure-activity relationship studies
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Dopamine receptors (DRs) are class A (rhodopsin-like) G protein-coupled receptors (GPCR), divided into D1-like (DRD1, DRD5) and D2-like (DRD2, DRD3, DRD4) subfamilies. They are widely distributed in the nervous system (CNS), playing crucial roles in locomotion, motivation, cognition, and endocrine function. Irregularities in dopaminergic signalling via DRs have been implicated in numerous CNS diseases, including, among others, neurological disorders (Parkinson’s disease, Huntington’s disease, schizophrenia), ADHD, and addictions (drugs, alcohol, food intake, etc.). Moreover, there is growing evidence linking DRs to cancer development, glioblastoma tumour progression in particular, as well as gastric cancer, breast cancer, lung cancer, acute myeloid leukemia and pancreatic cancer. Due to their involvement in such a wide variety of diseases, DRs have become attractive targets in research. However, the development of effective and selective DR ligands faces challenges including achieving desired subtype selectivity due to high homology between different DR subtypes, managing off-target effects, and ensuring adequate pharmacokinetic properties for oral bioavailability and CNS penetration. Other challenges involve inconclusive evidence or contradictory information pertaining to the role of DRs in tumour treatment, as well as different expression levels of DRs in different tumour subtypes. Currently, novel approaches are being employed to develop selective or multi-target compounds, bitopic ligands, degraders for targeted protein degradation (PROTACs) and others, as well as to understand the involvement of DRs in different pathologies. In silico and molecular modelling approaches are used in the design and understanding of DR-related selectivity and ligand interactions.
In this Special Issue, we aim to address these novel approaches to reflect on the current state of the art in the field of DR-drug development. Other approaches, such as those involving the analysis of drug-like properties (DMPK analyses) and interdisciplinary studies (use of artificial intelligence software, etc.) are welcome as well. We welcome submissions of original works, as well as review articles.
Dr. Pegi Pavletić
Dr. Fabio Del Bello
Guest Editors
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Keywords
- dopamine receptors (DRs)
- GPCR
- drug discovery
- in silico drug design
- drug optimization
- molecular modelling
- targeted protein degradation
- DMPK
- neurological disorders
- cancer
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